scholarly journals The Protective Potential of Metformin against Liver Acetaminophen Toxicity

2021 ◽  
Vol 11 (3) ◽  
Author(s):  
Dina Suhail
Keyword(s):  
Antioxidant Enzymes ◽  
Cell Viability ◽  
Hepg2 Cells ◽  
Reduced Glutathione ◽  
Membrane Integrity ◽  
Therapeutic Interventions ◽  
Viability Assessment ◽  
Metabolic Intermediate ◽  
Acetaminophen Toxicity

The inadequacy to replace acetaminophen (APAP) with a more effective analgesic continues its use in therapeutic interventions, upholding the risk of hepatotoxicity. Depletion of glutathione reserves by a metabolic intermediate of acetaminophen, N-acetyl-p-benzoquinone imine (NAPQI), is the major reason. The current study presents the combinatorial effect of metformin, a biguanide, in ameliorating the APAP toxicity. HepG2 cells were used for in vitro studies and MTT and LDH leakage assays were used for viability assessment. 10 ?M of metformin improved the cell viability and membrane integrity of cells treated with a high antioxidant enzymes and reduced glutathione were significantly increased in cells co-administrated with metformin and acetaminophen

scholarly journals Biological Effects of XyloCore, a Glucose Sparing PD Solution, on Mesothelial Cells: Focus on Mesothelial-Mesenchymal Transition, Inflammation and Angiogenesis

Nutrients ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 2282
Author(s):  
Valentina Masola ◽  
Mario Bonomini ◽  
Maurizio Onisto ◽  
Pietro Manuel Ferraro ◽  
Arduino Arduini ◽  
...  
Keyword(s):  
Endothelial Cell ◽  
Cell Viability ◽  
Biological Effects ◽  
Membrane Integrity ◽  
Glucose Content ◽  
Mesenchymal Transition ◽  
Low Glucose ◽  
Endothelial To Mesenchymal Transition ◽  
Osmotic Agents

Glucose-based solutions remain the most used osmotic agents in peritoneal dialysis (PD), but unavoidably they contribute to the loss of peritoneal filtration capacity. Here, we evaluated at a molecular level the effects of XyloCore, a new PD solution with a low glucose content, in mesothelial and endothelial cells. Cell viability, integrity of mesothelial and endothelial cell membrane, activation of mesothelial and endothelial to mesenchymal transition programs, inflammation, and angiogenesis were evaluated by several techniques. Results showed that XyloCore preserves mesothelial and endothelial cell viability and membrane integrity. Moreover XyloCore, unlike glucose-based solutions, does not exert pro-fibrotic, -inflammatory, and -angiogenic effects. Overall, the in vitro evidence suggests that XyloCore could represent a potential biocompatible solution promising better outcomes in clinical practice.

scholarly journals Antitumor Effect of the Essential Oil from the Leaves of Croton matourensis Aubl. (Euphorbiaceae)

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2974 ◽  
Author(s):  
Emilly Lima ◽  
Rafaela Alves ◽  
Gigliola D´Elia ◽  
Talita Anunciação ◽  
Valdenizia Silva ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Essential Oil ◽  
Cancer Cell ◽  
Hepg2 Cells ◽  
Membrane Integrity ◽  
In Vitro Cytotoxicity ◽  
Cell Cycle Distribution ◽  
Antitumor Effects

Croton matourensis Aubl. (synonym Croton lanjouwensis Jabl.), popularly known as “orelha de burro”, “maravuvuia”, and/or “sangrad’água”, is a medicinal plant used in Brazilian folk medicine as a depurative and in the treatment of infections, fractures, and colds. In this work, we investigated the chemical composition and in vitro cytotoxic and in vivo antitumor effects of the essential oil (EO) from the leaves of C. matourensis collected from the Amazon rainforest. The EO was obtained by hydrodistillation using a Clevenger-type apparatus and characterized qualitatively and quantitatively by gas chromatography coupled to mass spectrometry (GC–MS) and gas chromatography with flame ionization detection (GC–FID), respectively. In vitro cytotoxicity of the EO was assessed in cancer cell lines (MCF-7, HCT116, HepG2, and HL-60) and the non-cancer cell line (MRC-5) using the Alamar blue assay. Furthermore, annexin V-FITC/PI staining and the cell cycle distribution were evaluated with EO-treated HepG2 cells by flow cytometry. In vivo efficacy of the EO (40 and 80 mg/kg/day) was demonstrated in C.B-17 severe combined immunodeficient (SCID) mice with HepG2 cell xenografts. The EO included β-caryophyllene, thunbergol, cembrene, p-cymene, and β-elemene as major constituents. The EO exhibited promising cytotoxicity and was able to cause phosphatidylserine externalization and DNA fragmentation without loss of the cell membrane integrity in HepG2 cells. In vivo tumor mass inhibition rates of the EO were 34.6% to 55.9%. Altogether, these data indicate the anticancer potential effect of C. matourensis.

scholarly journals In Vitro Protective Effect of Paste and Sauce Extract Made with Protaetia brevitarsis Larvae on HepG2 Cells Damaged by Ethanol

Insects ◽  
2020 ◽  
Vol 11 (8) ◽  
pp. 494 ◽  
Author(s):  
Dooseon Hwang ◽  
Tae-Won Goo ◽  
Eun-Young Yun
Keyword(s):  
Hepg2 Cells ◽  
Tumor Necrosis ◽  
Reduced Glutathione ◽  
Fermented Food ◽  
Inhibition Rate ◽  
Tnf Α ◽  
Antioxidative Effects ◽  
Protein Rich ◽  
Necrosis Factor

We made paste and sauce using protein-rich Protaetia brevitarsis larvae (PBL) and evaluated their fermentation levels. After pretreatment with the paste and sauce extracts, HepG2 cells were damaged with ethanol (EtOH), and then the effects of the paste and sauce were evaluated. As a result, we confirmed that the PBL paste and sauce extracts reduced the aspartate aminotransferase (AST) and alanine aminotransaminase (ALT) content in the medium as compared to soybean (Glycine max) sauce and paste extracts. In addition, the PBL paste and sauce extracts significantly lowered the level of tumor necrosis factor (TNF)-α and interleukin (IL)-6, which are biomarkers of inflammation, and significantly increased the inhibition rate of superoxide dismutase (SOD) and reduced glutathione (GSH), which are antioxidative indicators, in proportion to the amount of PBL added to the paste and sauce. These results suggest that an intake of PBL paste and sauce, a novel type of fermented food made from insects, may be effective for liver protection through anti-inflammatory and antioxidative effects against hepatocyte injury caused by EtOH.

scholarly journals Assessment of in-vitro Antioxidant/Enzymes Inhibitory Potentials of Aframomum melegueta [Roscoe] K. Schum (Grains of Paradise) Leaf, Stem Bark, Seed Bark and Seed Extracts

2020 ◽  
pp. 40-57
Author(s):  
Oludare Temitope Osuntokun ◽  
V. O. Olumekun ◽  
A. O. Ajayi ◽  
I. O. Omotuyi ◽  
A. Olonisakin
Keyword(s):  
Superoxide Dismutase ◽  
Antioxidant Enzymes ◽  
Free Radical ◽  
Reduced Glutathione ◽  
Research Work ◽  
Radical Scavenging ◽  
Stem Bark ◽  
Oh Radical ◽  
Seed Extracts

The purpose of this research work is to evaluates the in-vitro antioxidant and antioxidant enzymes inhibition potentials of Aframomum melegueta [Roscoe] K. Schum (Grains of Paradise) Leaf, Stem Bark, Seed Bark and Seed Extracts. Aframomum melegueta is a spice with a similar composition as Ginger, that belongs to the same Zingiberaceae family, used in Nigeria, West Africa and it is used for the treatment of infectious diseases such as urinary tract infections, cancer and diabetes. Antioxidants neutralize the effect of free radicals through different ways and may prevent the body from various diseases. The plant extract were collected from a rain forest in Akugba Akoko, Ondo state, Nigeria. The plant sample was dried, pulverized, filtered with Whatman No 1 filtered paper and the filtrates was concentrated in-vacuum using vacuum rotary evaporator at 40°C and was later concentrated to dryness in a hot-air oven at 40°C. Assessment of antioxidant potentials were performed using Singleton method Total flavonoids (mg/g), Phenol (mg/g), Ferric reducing (FRAP) potentials (mg/g), Free radical scavenging ability (DPPH) (1, 1- diphenyl-2-picryhydrazyl) potentials (%),2,2’-azino-bis(3-ethylbenthiazoline-6-sulphonic acid), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) scavenging potentials (mMol/g), Fe2+ chelation potentials (%) and OH Radical Scavenging potentials (%) were evaluated. Antioxidant enzymes of plant were assessed using Bentller method, Superoxide Dismutase (SOD) (%), Reduced Glutathione (GSH) (%), Catalase (CAT) and Glutathione Peroxidise (GPX) were evaluated. Seed extract among other extracts of Aframomum melegueta has the highest quantity of flavonoids, Phenol, FRAP, DPPH, ABTS, Fe2+ chelation and OH radical scavenging potential. The leaf extract of A. meleguata has the highest percentage of Superoxide Dismutase (SOD) and Catalase (CAT) while stem bark of Aframomum melegueta has the highest percentage of Reduced Glutathione (GSH) and Glutathione Peroxidise (GPX).it can be deduced from this research work that all parts of the A. melegueta has pharmacological and therapeutic activities judging from literature that A. melegueta can be used to prevent oxidative damage by ROS (Reactive oxygen species) reacting with free radical chelating and catalytic metals  which can be used to reduce and prevent various diseases like heart disease, cancer, DNA degeneration, pulmonary and neurological disorder. SOD, GPX, GSH help to control cytokins induced peroxidise level and mediate signal transduction in mammalian cells. It can be deduced that Aframomum melegueta should be the focal point in human diet, natural herbal drug supplement and even in addition to conventional drug to improve the potency and quality of natural drug system. The use of Aframomum melegueta should be encouraged. These results show the potential of Aframomum melegueta as a source of bioactive compounds to be used for pharmaceutical, nutraceutical, and cosmeceutical applications.

scholarly journals Polystyrene nanoplastics and microplastics can act as Trojan horse carriers of benzo(a)pyrene to mussel hemocytes in vitro

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Alberto Katsumiti ◽  
María Paula Losada-Carrillo ◽  
Marta Barros ◽  
Miren P. Cajaraville
Keyword(s):  
Plasma Membrane ◽  
Cell Viability ◽  
Phagocytic Activity ◽  
Membrane Integrity ◽  
Aquatic Organisms ◽  
Particle Aggregation ◽  
Ros Production ◽  
Plasma Membrane Integrity ◽  
Intracellular Fate

AbstractIn this work we studied the ability of polystyrene (PS) nanoplastics (NPs) and microplastics (MPs) to transfer benzo(a)pyrene (BaP) to mussel hemocytes and to produce toxic effects in vitro. For this, intracellular fate and toxicity of PS NPs (0.05 μm) and MPs (0.5 and 4.5 μm) alone or with BaP and of BaP alone were assessed. Particles of 0.05 and 0.5 µm largely aggregated in the exposure medium whereas presence of BaP reduced particle aggregation. Cells internalized PS NPs and MPs alone or with BaP and these were found inside and outside lysosomes, depending on their size. PS particles alone or with BaP were cytotoxic to hemocytes only at the highest concentrations tested. The same was true for most sublethal endpoints except for increased phagocytic activity provoked by NPs and 0.5 μm MPs at lower concentrations. Plastic particles appeared to be the main drivers for reduced plasma membrane integrity and increased phagocytic and lysosomal activities whereas BaP appeared to contribute more to reduced cell viability and phagocytosis and increased ROS production and genotoxicity. Overall, PS NPs and MPs can act as carriers of BaP to mussel hemocytes, rising concerns about risks plastics associated to pollutants may pose to aquatic organisms.

Non-Clinical investigation of Tuberculosis Drugs - Conjugated Norbornene-Based Nanocarriers Toxic Impacts on Zebrafish

2021 ◽  
Vol 12 ◽  
Author(s):  
Thangammal Anju ◽  
Radhakrishnan Preetha ◽  
Raja Shunmugam ◽  
Shivshankar R Mane ◽  
Jesu Arockiaraj ◽  
...  
Keyword(s):  
Dna Damage ◽  
Cell Viability ◽  
Hepg2 Cells ◽  
In Vitro Study ◽  
Liver Cells ◽  
Vitro Study ◽  
Ros Generation ◽  
Human Liver Cell ◽  
Zebrafish Liver

INTRODUCTION: Rifampicin conjugated (R-CP), and rifampicin -isoniazid dual conjugated (RI-CP) norbornene-derived nanocarriers are newly designed for pH stimuli-responsive delivery of tuberculosis (TB) drugs. Its biosafety level is yet to be well established. OBJECTIVES: To assess the impacts of the nanocarriers on liver cells using zebrafish animal model and human liver cell line model (HepG2). METHODS: Initially, lethal dose concentration for the norbornene-derived nanocarrier systems in zebrafish was determined. The toxic effects were analysed at the sub-lethal drug concentration by histopathological study, total GSH level, gene expression and DNA damage in zebrafish liver cells. Fish erythrocyte nuclear abnormalities were also evaluated. Cell viability and oxidative stress level (ROS generation) after exposure to the nanoconjugates was determined using HepG2 cell in the in vitro study. RESULTS: In vivo studies of both R-CP and RI-CP showed 100% mortality at 96 hours for exposure concentration >100mg/l and showed toxic changes in zebrafish liver histology, GSH, and DNA damage levels. A noticeable upregulated PXR, CYP3A and cyp2p6 genes was observed in RI-CP exposure than in RIF or R-CP molecules. The in vitro study revealed a dose-dependent effect on cell viability and ROS generation for RIF, R-CP and RI-CP exposures in HepG2 cells. CONCLUSION: The current study reports that the rifampicin conjugated (R-CP) and rifampicin-isoniazid conjugated (RI-CP) norbornene derived nanocarriers exhibit enhanced toxic responses in both adult zebrafish and HepG2 cells. The pH-sensitive norbornene derived nanocarriers on conjugation with different drugs exhibited varied impacts on hepatic cells. Hence the present investigation recommends a complete metabolomics analysis and norbornene carrier-drug interaction study to be performed for each drug conjugated norbornene nanocarrier to ensure its biosafety.

scholarly journals Sex steroids differentially regulate fshb, lhb and gnrhr expression in Atlantic cod (Gadus morhua)

Reproduction ◽  
2017 ◽  
Vol 154 (5) ◽  
pp. 581-594 ◽  
Author(s):  
Kristine von Krogh ◽  
Gunnveig Toft Bjørndal ◽  
Rasoul Nourizadeh-Lillabadi ◽  
Kjetil Hodne ◽  
Erik Ropstad ◽  
...  
Keyword(s):  
Gene Expression ◽  
Cell Viability ◽  
Gadus Morhua ◽  
Hormone Receptors ◽  
Atlantic Cod ◽  
Membrane Integrity ◽  
Gonad Maturation ◽  
Maturity Stage ◽  
Its Gene

Depending on the stage of gonad maturation, as well as other factors, gonadal steroids can exert either a positive or negative feedback at the brain and pituitary level. While this has been demonstrated in many teleost species, little is known about the nature of steroid feedback in Gadiform fish. Using an optimized in vitro model system of the Atlantic cod pituitary, the present study investigated the potential effects of two physiologically relevant doses of estradiol, testosterone (TS) or dihydrotestosterone (DHTS) on cell viability and gene expression of gonadotropin subunits (fshb/lhb) and two suggested reproduction-relevant gonadotropin-releasing hormone receptors (gnrhr1b/gnrhr2a) during three stages of sexual maturity. In general, all steroids stimulated cell viability in terms of metabolic activity and membrane integrity. Furthermore, all steroids affected fshb expression, with the effect depending on both the specific steroid, dose and maturity status. Conversely, only DHTS exposure affected lhb levels, and this occurred only during the spawning season. Using single-cell qPCR, co-transcription of gnrhr1b and gnrhr2a was confirmed to both fshb- and lhb- expressing gonadotropes, with gnrhr2a being the most prominently expressed isoform. While steroid exposure had no effect on gnrhr1b expression, all steroids affected gnrhr2a transcript levels in at least one maturity stage. These and previous results from our group point to Gnrhr2a as the main modulator of gonadotropin regulation in cod and that regulation of its gene expression level might function as a direct mechanism for steroid feedback at the pituitary level.

scholarly journals NOVEL UMBELLIFERONE PHYTOSOMES: DEVELOPMENT AND OPTIMIZATION USING EXPERIMENTAL DESIGN APPROACH AND EVALUATION OF PHOTO-PROTECTIVE AND ANTIOXIDANT ACTIVITY

2016 ◽  
Vol 9 (1) ◽  
pp. 218 ◽  
Author(s):  
Parul A. Ittadwar ◽  
Prashant K. Puranik
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Enzymes ◽  
Partition Coefficient ◽  
Ex Vivo ◽  
Reduced Glutathione ◽  
Pharmacological Action ◽  
Box Behnken Design ◽  
Coefficient Method ◽  
Better Than

<p><strong>Objective: </strong>The objective of this study was to develop a novel formulation (Phytosome) of umbelliferone with phospholipid for improved permeability, solubility and hence better pharmacological action.</p><p><strong>Methods: </strong>The phytosomal complex was prepared by using solvent evaporation method and optimised by applying the Box-Behnken design on the basis of complexation rate and partition coefficient. The formation of phytosomes was confirmed by FTIR, DSC, SEM, XRD, HPTLC and NMR by comparing the results of the complex with the drug. The photoprotective potential of complex against UV-exposure was evaluated in rats and compared with the drug by incorporating it in a gel and estimating the antioxidant enzymes in skin namely reduced glutathione, superoxide dismutase, lipid peroxidation and catalase.</p><p><strong>Results: </strong>The crystalline drug was completely converted to amorphous complex. The complex showed a good practical yield, drug content and particle size was in the range. The solubility of the complex was determined by partition coefficient method and was found to be better than the drug. The <em>ex vivo</em> and <em>in-vitro</em> permeation of the complex showed improved permeation for complex than the drug. The <em>in vitro</em> antioxidant activity of complex was evaluated by DPPH and ferrozine antioxidant assay and was better than the drug. The photoprotective action of the complex was found to be better than drug on the basis of the content of antioxidant enzymes estimated in the skin.</p><strong>Conclusion: </strong>The phytosomal complex was found to show better solubility in the water phase and oil phase, better permeation, better antioxidant activity and a better photo-protective activity when compared to umbelliferone.

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